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Scott A Watkins

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Articles 12
Citations 108
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Recent Articles
1.
Hamdouchi C, Zhong B, Mendoza J, Collins E, Jaramillo C, Diego J, et al.
Bioorg Med Chem Lett . 2005 Mar; 15(7):1943-7. PMID: 15780638
Structure-based design approach was successfully used to guide the evolution of imidazopyridine scaffold yielding new structural class of highly selective inhibitors of cyclin dependent kinases that were able to form...
2.
Peng S, Yan L, Xia X, Watkins S, Brooks H, Beight D, et al.
Biochemistry . 2005 Feb; 44(7):2293-304. PMID: 15709742
Transforming growth factor beta (TGF-beta) signaling pathways regulate a wide variety of cellular processes including cell proliferation, differentiation, extracellular matrix deposition, development, and apoptosis. TGF-beta type-I receptor (TbetaRI) is the...
3.
Jaramillo C, de Diego J, Hamdouchi C, Collins E, Keyser H, Sanchez-Martinez C, et al.
Bioorg Med Chem Lett . 2004 Nov; 14(24):6095-9. PMID: 15546737
We have identified a novel structural class of protein serine/threonine kinase inhibitors comprised of an aminoimidazo[1,2-a]pyridine nucleus. Compounds from this family are shown to potently inhibit cyclin-dependent kinases by competing...
4.
Al-Awar R, Ray J, Hecker K, Joseph S, Huang J, Shih C, et al.
Bioorg Med Chem Lett . 2004 Jul; 14(15):3925-8. PMID: 15225699
The synthesis of novel aza-1,7-annulated indoles was achieved and these were converted to indolocarbazoles that proved to be potent kinase inhibitors. These compounds were also evaluated in a human colon...
5.
Al-Awar R, Ray J, Hecker K, Huang J, Waid P, Shih C, et al.
Bioorg Med Chem Lett . 2004 May; 14(12):3217-20. PMID: 15149678
The synthesis and kinase inhibitory activity of a series of novel 1,7-annulated indolocarbazoles 6 and 16 is described. These compounds exhibited potent inhibitory activity against cyclin-dependent kinase 4 and good...
6.
Zhu G, Conner S, Zhou X, Chan H, Shih C, Engler T, et al.
Bioorg Med Chem Lett . 2004 May; 14(12):3057-61. PMID: 15149644
The synthesis of a novel series of 1,7-annulated indolocarbazoles 2 and 16 is described. These compounds were found to be potent cyclin dependent kinase inhibitors with good antiproliferative activity against...
7.
Hamdouchi C, Keyser H, Collins E, Jaramillo C, Diego J, Spencer C, et al.
Mol Cancer Ther . 2004 Jan; 3(1):1-9. PMID: 14749470
The protein kinase family represents an enormous opportunity for drug development. However, the current limitation in structural diversity of kinase inhibitors has complicated efforts to identify effective treatments of diseases...
8.
Sanchez-Martinez C, Shih C, Zhu G, Li T, Brooks H, Patel B, et al.
Bioorg Med Chem Lett . 2003 Oct; 13(21):3841-6. PMID: 14552792
A series of indolo[2,3-a]pyrrolo[3,4-c]carbazoles and their bis-indolylmaleimides precursors have been prepared in order to compare their activity as D1-CDK4 inhibitors. Both enzymatic and antiproliferative assays have shown that the structurally...
9.
Sanchez-Martinez C, Shih C, Faul M, Zhu G, Paal M, Somoza C, et al.
Bioorg Med Chem Lett . 2003 Oct; 13(21):3835-9. PMID: 14552791
The synthesis of new analogues of Arcyriaflavin A in which one indole ring is replaced by an aryl or heteroaryl ring is described. These new series of aryl[a]pyrrolo[3,4-c]carbazoles were evaluated...
10.
Engler T, Furness K, Malhotra S, Sanchez-Martinez C, Shih C, Xie W, et al.
Bioorg Med Chem Lett . 2003 Jun; 13(14):2261-7. PMID: 12824014
The synthesis and CDK inhibitory properties of a series of indolo[6,7-a]pyrrolo[3,4-c]carbazoles is reported. In addition to their potent CDK activity, the compounds display antiproliferative activity against two human cancer cell...